Highly Active Analogs of alpha-Factor and Their Activities Against Saccharomyces cerevisiae

Title
Highly Active Analogs of alpha-Factor and Their Activities Against Saccharomyces cerevisiae
Author(s)
홍남주안희준홍은영[홍은영]진동훈[진동훈]
Keywords
PROTEIN-COUPLED RECEPTOR; TRIDECAPEPTIDE MATING PHEROMONE; SOLID-PHASE SYNTHESIS; CONFORMATIONAL-ANALYSIS; PEPTIDE AGONISTS; LIGAND-BINDING; CROSS-LINKING; A-CELLS; STE2P; ENKEPHALIN
Issue Date
201405
Publisher
KOREAN CHEMICAL SOC
Citation
BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.35, no.5, pp.1365 - 1374
Abstract
Thirteen analogs of tridecapeptide alpha-factor (WHWLQLKPGQPMY) of Saccharomyces cerevisiae with C- or N-terminal Trp extension and isosteric replacement by Aib at position 8 and 11, Trp at position 13, D-Ala at position 9, and Orn and Glu at position 6 were synthesized and assayed for their biological activity. Receptor binding assay was carried out using our newly developed spectrophotometric method with detector peptide 14. C- or N-terminal extended analogs, alpha-factor-[Trp](n) (n=1-5) 1-5 and [N-Trp](i)-alpha-factor 6, were all less active than native alpha-factor and gradual decreases in both activity and receptor affinity were observed with greater Trp extension. Trp-substituted analog at position 13, [Trp(13)] alpha-factor 7, exhibited about 2-fold reductions in both activity and receptor affinity. Aib-substituted analogs, [Aib(8)]alpha-factor 8 and [Aib(11)]alpha-factor 9, showed 5- to 10-fold reduction in activity as well as 3-fold reduction in receptor affinity compared to native alpha-factor. [Orn(6)]alpha-factor 10 demonstrated strong potency with a 7.0-fold increase in halo activity as well as 1.8-fold increase in receptor affinity compared to native alpha-factor. For two double substituted analogs, [Glu(6),D-Ala(9)]alpha-factor 12 showed the slightly decreased potency in halo activity compared to analog 10, whereas [Orn(6),D-Ala(9)]alpha-factor 11 exhibited 15-fold higher halo activity as well as nearly 3-fold higher receptor affinity compared to native alpha-factor.
URI
http://hdl.handle.net/YU.REPOSITORY/32287http://dx.doi.org/10.5012/bkcs.2014.35.5.1365
ISSN
0253-2964
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